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An acute exacerbation of COPD is a sudden worsening of COPD symptoms (shortness of breath, quantity and color of phlegm) that typically lasts for several days. It may be triggered by an infection with bacteria or viruses or by environmental pollutants. Typically, infections cause 75% or more of the exacerbations; bacteria can roughly be found in 25% of cases, viruses in another 25%, and both viruses and bacteria in another 25%

Drugs used in bronchial asthma

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Bronchial Asthma• Asthma as an inflammatory illness• Accounting 5000 deaths/ year in USA• Asthma is common disorder and it is characterized by airwayinflammation and hyperresponsiveness to stimuli that producebronchoconstriction. These stimuli include cold air, exercise, a widevariety of allergens and emotional stress.– Extrinsic asthma: It is mostly episodic, less prone to statusasthmaticus.– Intrinsic asthma: It tends to be perennial, status asthmaticus is morecommon.

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Sympathomimetics• Bambuterol:– Biocarbamate ester of prodrug of terbutaline– Slowly hydrolyzed in plasma and lung by pseudocholinesterase to release theactive drug over 24 h. It also reversely inhibits pseudocholinesterasein a dosedependent mannor.– Used in chronic bronchial asthma in a singe evening dose of 10-20 mg/ oral.• Salmeterol:– First long acting selective β2 agonists with slow onset of action– Twice daily for maintain the therapy/ nocturnal asthma, but not for acute asthma– Concurrent use of inhaled glucocorticoid with salmeterol is advised for patientwith persistent asthma.– COPD: equivalent to inhaled anticholinergics in COPD. Reduce breathlessness byabolishing the reversible component of airway obstruction.• Formoterol:– Long acting selective β2 agonists which acts 12 h when inhaled.– Compare to salmeterol it has a faster onset of action (with in 10 min)Cont.,

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Methylxanthines• Theophylline and its derivatives are most commonly used for thetreatment of COPD and asthma.• Caffeine, theophylline and theobromine are naturally occurring xanthinealkaloids which have qualitatively similar actions.• Mechanism of action:– Methylxanthines inhibits cyclic nucleotide phosphodiesterase(PDEs), thereby preventing conversion of cAMP and cGMP to 5’-AMP and5’-GMP, respectively. Inhibition of PDEs will lead to an accumulation ofintracellular cAMP and cGMP. Bronchodilataion, cardiac stimulation andvasodilatation occur when cAMP level rises in the concerned cells.Theophylline and related methylxanthines are relatively nonselective in thePDE subtypes inhibitor.– Theophylline is a competitive antagonist at adenosine receptors.Adenosine can cause bronchoconstriction in asthmatics and potentiateimmunologically induced mediator release from human lung mast cells.Methylxanthines inhibits the adenosine action thereby casingbronchodilataion.

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Leukotriene antagonistsMontelukast, Zafirlukast• Both are having similar action and clincial utility• Block the cys-leukotrienes C4, D4 and E4 (LTC4, LTD4, LTE4)• Alternative for inhaled glucocorticoids• Prophylactic therapy for mild, moderate asthma; not used forterminating asthma.• Both are very safe drugs and ADRs are few (headache, rashes);eosinophilia and neuropathy are infrequent. Few cases Churg-Strausssyndrome (vasculitis with eosinophilia) have been reported.• Dose: Montelukast 10 mg OD, Zafirlukast 20 mg BD

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Mast cell stabilizersSodium cromoglycate, Ketotifen• Inhibits degranulation of mast cell by trigger stimuli and prevent therelease of histamine, LTs, PAF, interleukins etc. from mast cells.Inhibition of mediator release by cromolyn is through blockade ofcalcium influx in mast cells.• Long time therapy reduce cellular inflammatory response.• It is not histamine antagonist/ bronchodilator- ineffective in asthmaticattack.• Pharmacokinetic:– Not absorbed orally. It is administered as an aerosol through metered doseinhaler delivering 1 mg per dose; 2 puffs 4 times a day– Not popular- production of cough and bronchospasm because of particulatenature of the inhalation.– Small fraction of the inhaled drug is absorbed systemically and excretedunchanged form in urine and bile.

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Anti-lgE antibody: Omalizumab• recombinant DNA-derived monoclonal antibody• Selectively binds to human immunoglobulin E (IgE) and decrease bindingaffinity of IgE to the high-affinity IgE receptor on the surface of mast cellsand basophils, reduce allergic response.• Omalizumab may be particularly useful for treatment of moderate to severeallergic asthma in patients who are poorly controlled with conventionaltherapy.• Due to the high cost of the drug, limitations on dosage, and limited clinicaltrial data, it is not currently used as firstline therapy.